tobramycin/loteprednol ophthalmic

Action and Spectrum

Actions and Spectrum: 

tobramycin/loteprednol ophthalmic is a combination medication used in ophthalmology to treat certain eye conditions and infections.  

Action: 

• tobramycin: It is an antibiotic that belongs to the class of aminoglycosides. It works by inhibiting bacterial protein synthesis, thereby killing or slowing the growth of susceptible bacteria. tobramycin has a broad-spectrum activity against various gram-positive and gram-negative bacteria. 
• loteprednol: It is a corticosteroid that has anti-inflammatory and immunosuppressive properties. It generally works by inhibiting the production of inflammatory mediators, reducing inflammation, and suppressing the immune response in the eye. 

The spectrum of activity: 

• tobramycin/loteprednol ophthalmic is primarily used to treat eye infections caused by susceptible bacteria. It is effective against both gram-positive and also gram-negative bacteria. 

The spectrum of activity may vary depending on the local resistance patterns in a specific geographical area. Therefore, susceptibility testing should be performed to identify the causative bacteria and determine their sensitivity to tobramycin. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Watery eyes 

Headache 

Puffy eyelids 

Enhanced sensitivity to light 

Stinging 

Burning 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

tobramycin/loteprednol ophthalmic should not be used in individuals with known hypersensitivity or allergy to tobramycin, loteprednol, or other medication components. 

Additionally, it is vital to consider the following contraindications: 

• Viral/fungal infections of the eye: tobramycin/loteprednol ophthalmic is an antibiotic-steroid combination used to treat eye bacterial infections. It is not effective against viral/fungal infections. Therefore, it should not be used in individuals with active viral or fungal eye infections. 
• Herpes simplex keratitis: tobramycin/loteprednol ophthalmic is not recommended for use in individuals with herpes simplex keratitis, a viral eye infection caused by the herpes simplex virus. Using steroids in these cases can exacerbate the infection and cause serious complications. 
• Mycobacterial infections: Individuals with mycobacterial infections of the eye, such as tuberculosis or other non-tuberculous mycobacterial infections, should not use tobramycin/loteprednol ophthalmic. Using steroids in these cases can lead to disease progression or dissemination. 
• Fungal keratitis: Fungal keratitis is a fungal infection of the cornea. tobramycin/loteprednol ophthalmic should be avoided in individuals with fungal keratitis as steroids can worsen fungal infections. 

Caution 

• Bacterial resistance: Prolonged use of antibiotics, including tobramycin, can result in the overgrowth of non-susceptible bacteria or fungi. If a secondary infection occurs during treatment, appropriate alternative therapy should be initiated. 
• Delayed healing: In the eye, corticosteroids, such as loteprednol, can delay wound healing. Therefore, tobramycin/loteprednol ophthalmic should be used cautiously in individuals with corneal or conjunctival epithelial defects or those with a history of corneal or scleral thinning. 
• Glaucoma: Corticosteroids can increase intraocular pressure in some individuals, potentially leading to glaucoma. Therefore, caution should be exercised in patients with a history of elevated intraocular pressure or glaucoma. Regular monitoring of intraocular pressure may be necessary during treatment. 
• Cataracts: Prolonged use of corticosteroids can lead to cataracts in susceptible individuals. This is more likely to occur with higher doses and longer treatment durations. 
• Contact lens use: Contact lenses should not be worn during treatment unless specifically instructed by the healthcare professional. loteprednol may contain benzalkonium chloride, which can be absorbed by the soft contact lenses and cause eye irritation. 
• Use in children: The safety and efficacy of tobramycin/loteprednol ophthalmic in pediatric patients have not been established.  

Pregnancy / Lactation

Pregnancy consideration: 

US FDA pregnancy category: C 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

tobramycin/loteprednol ophthalmic is a combination medication that combines the antibiotic tobramycin and the corticosteroid loteprednol. tobramycin belongs to the aminoglycoside class of antibiotics and works by inhibiting bacterial protein synthesis, thereby preventing the growth and killing of susceptible bacteria.

loteprednol is a corticosteroid that has anti-inflammatory and immunosuppressive properties. It typically acts by inhibiting the production of inflammatory mediators and suppressing the immune response in the eye. Combining tobramycin and loteprednol provides antimicrobial activities against bacterial infections and inflammation control, effectively treating bacterial eye infections and reducing ocular inflammation. 

Pharmacodynamics: 

Mechanism of action: tobramycin/loteprednol ophthalmic involves the individual actions of its two components, tobramycin and loteprednol. 

• tobramycin: tobramycin is an antibiotic that belongs to the aminoglycoside class. It works by inhibiting bacterial protein synthesis. Specifically, tobramycin binds to the 30S ribosomal subunit of bacteria, disrupting functional ribosome formation. This inhibition prevents the bacteria from synthesizing essential proteins, leading to impaired growth and, eventually, bacterial cell death. tobramycin has a broad-spectrum activity against gram-positive and gram-negative bacteria, including those commonly associated with eye infections. 
• loteprednol: loteprednol is a corticosteroid that possesses anti-inflammatory and immunosuppressive properties. It typically acts by inhibiting the synthesis of inflammatory mediators such as prostaglandins, leukotrienes, and various cytokines. By suppressing inflammation, loteprednol helps to reduce swelling, redness, and discomfort in the eye. It also inhibits the migration of the inflammatory cells into the ocular tissues and modulates the immune response, thus further contributing to its anti-inflammatory effects. 

Pharmacokinetics: 

Absorption 

When tobramycin/loteprednol ophthalmic is administered as eye drops, both tobramycin and loteprednol can be absorbed systemically. However, systemic absorption is minimal compared to oral or systemic administration of these drugs. 

Distribution 

tobramycin has a relatively large volume of distribution and can penetrate ocular tissues, including the cornea and aqueous humor. loteprednol, being a corticosteroid, can also distribute into ocular tissues and exert its anti-inflammatory effects locally. 

Metabolism 

tobramycin is primarily eliminated unchanged by the kidneys and undergoes minimal metabolism. On the other hand, loteprednol undergoes extensive metabolism in the liver to inactive metabolites. This metabolism reduces systemic exposure to loteprednol, which helps minimize systemic side effects. 

Elimination and Excretion 

tobramycin is mainly excreted unchanged in the urine. loteprednol and its metabolites are eliminated mainly through urine and feces. 

Adminstartion

Administration: 

Ophthalmic administration 

tobramycin/loteprednol ophthalmic is typically administered as eye drops. It is essential to follow your healthcare professional or pharmacist’s instructions.  

• Wash your hands thoroughly before handling the eye drops to prevent contamination. 
• Shake the eye drop bottle gently before use, if required, to ensure proper medication mixing. 
• Tilt your head back or lie down, and gently pull down lower eyelid to create a tiny pocket. 
• Hold the eye drop bottle upside down, close to your eye, without touching your eye or any other surface. 
• Squeeze the bottle and instill the prescribed number of drops into the pocket created by pulling down the lower eyelid. Avoid blinking or squeezing your eyelids tightly while instilling the drops. 
• Release the lower eyelid and gently close your eyes. Do not rub your eyes. 
• If you are using other eye medications, wait at least 5 minutes before instilling them unless directed by your healthcare professional. 
• Replace and tighten the cap of the eye drop bottle immediately after use to prevent contamination. 
• If you use eye drops in both eyes, repeat the process for the other eye. 
• Rewash your hands to remove any residual medication. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tobramycin/loteprednol ophthalmic 

Pronounced: [ LOE-te-PRED-nol-and-TOE-bra-MYE-sin-off-THAL-mik ] 

Why do we use tobramycin/loteprednol ophthalmic? 

tobramycin/loteprednol ophthalmic is a combination medication used in ophthalmology to treat certain eye conditions. Here are some common uses of tobramycin/loteprednol ophthalmic: 

• Bacterial eye infections: tobramycin/loteprednol ophthalmic is primarily used to treat eye bacterial infections. It is effective against many gram-positive and gram-negative bacteria, including Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus influenzae, Escherichia coli, Proteus species, and Pseudomonas aeruginosa. 
• Ocular inflammation: loteprednol, one of the components of the medication, is a corticosteroid with anti-inflammatory properties. tobramycin/loteprednol is ophthalmic and is used to reduce inflammation in various eye conditions, such as allergic conjunctivitis, anterior uveitis, and postoperative inflammation following eye surgery.